Aurora kinases as targets for cancer therapy
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Updated: Jul 10, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Giannis Mountzios1, Evangelos Terpos, Meletios-Athanassios Dimopoulos
1Department of Medical Oncology, 251 General Airforce Hospital, Athens, Greece. gmountzios@med.uoa.gr
Abstract:
Aurora kinases represent a family of serine/threonine kinases highly conserved during evolution, whose main function is to promote mitotic spindle assembly by regulating centrosome duplication and separation. Inhibition of Aurora kinase activity may lead to defects in centrosome function, misaligned sister chromatids, mitotic spindle malformation, problematic cytokinesis and eventually mitotic arrest. Aurora kinases are overexpressed in a variety of tumor cell lines, suggesting their potential role in tumorigenesis and indicating that they could represent an appealing target for molecular therapies. Extensive pre-clinical information supports the development of Aurora kinase inhibitors in specific tumor types and a number of these novel agents are currently being extensively studied in phase I and II clinical trials exhibiting an acceptable toxicity profile and promising clinical efficacy. The current study aims to provide a comprehensive overview of the development of Aurora kinases as molecular targets for anticancer therapy by focusing on their physiological role in mitosis, their implication in oncogenesis and the potential ways of inhibiting their activity. The main pre-clinical and clinical studies concerning Aurora kinase inhibitors currently under investigation are reported and important considerations for their future development are discussed.
Insights
Aurora kinases are crucial for cell division and are often overexpressed in cancers. Inhibiting these kinases shows promise as a new anticancer therapy, with several drugs in clinical trials.
Area of Science:
- Molecular Biology
- Cell Biology
- Oncology
Background:
- Aurora kinases are serine/threonine kinases essential for mitotic spindle assembly and cell division.
- Overexpression of Aurora kinases is observed in various tumor cell lines, implicating them in tumorigenesis.
- These kinases regulate critical processes like centrosome duplication, separation, and cytokinesis.
Purpose of the Study:
- To provide a comprehensive overview of Aurora kinases as molecular targets for anticancer therapy.
- To discuss their physiological role in mitosis and implications in oncogenesis.
- To review pre-clinical and clinical studies of Aurora kinase inhibitors.
Main Methods:
- Review of existing literature on Aurora kinase biology and inhibitors.
- Analysis of pre-clinical data supporting Aurora kinase inhibitors.
- Summary of ongoing phase I and II clinical trials for Aurora kinase inhibitors.
Main Results:
- Inhibition of Aurora kinase activity can lead to mitotic arrest and cell death.
- Aurora kinase inhibitors have demonstrated acceptable toxicity profiles and promising efficacy in early clinical trials.
- Extensive pre-clinical evidence supports their development for specific tumor types.
Conclusions:
- Aurora kinases represent a promising target for novel anticancer therapies.
- Further development of Aurora kinase inhibitors is warranted based on current pre-clinical and clinical data.
- Understanding their role in mitosis and oncogenesis is key to optimizing therapeutic strategies.
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